Synthesis and biological evaluation of new HIV-1 protease inhibitors with purine bases as P2-ligands.
Bioorg Med Chem Lett
; 29(12): 1541-1545, 2019 06 15.
Article
em En
| MEDLINE
| ID: mdl-31014912
ABSTRACT
Introducing purine bases to P2-ligands might enhance the potency of Human Immunodeficiency Virus-1 (HIV-1) protease inhibitory because of the carbonyl and NH groups promoting the formation of extensive H-bonding interactions. In this work, thirty-three compounds are synthesized and evaluated, among which inhibitors 16a, 16f and 16j containing N-2-(6-substituted-9H-purin-9-yl)acetamide as the P2-ligands along with 4-methoxylphenylsulfonamide as the P2'-ligand, display potent inhibitory effect on the activity of HIV-1 protease with IC50 43â¯nM, 42â¯nM and 68â¯nM in vitro, respectively.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Purinas
/
Inibidores da Protease de HIV
/
Ligantes
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2019
Tipo de documento:
Article
País de afiliação:
China